[MePhe7]-Neurokinin B
Based on 1 Customer Validation
[MePhe7]-Neurokinin B is an neurokinin NK-3 receptor (NK3R) agonist with an IC50 value of 3 nM. [MePhe7]-Neurokinin B is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.76%
- CAS No.: 110880-53-0
- 화학식: C60H81N13O14S2
- 분자량:1272.49
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보관:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
![[MePhe7]-Neurokinin B Chemical Structure](https://file.medchemexpress.com/product_pic/hy-p3862.gif "Click to View [MePhe7]-Neurokinin B Chemical Structure")
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
NK3R 3 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.013 nM
Compound: 1a, [MePhe7]-NKB
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Agonist activity at NK3R (unknown origin) transfected in CHO cells assessed as calcium influx at 10 mM
Agonist activity at NK3R (unknown origin) transfected in CHO cells assessed as calcium influx at 10 mM
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[PMID: 23473945] |
| CHO | EC50 |
0.064 μM
Compound: [MePhe7]-NKB
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Agonist activity at human NK3R expressed in CHO cells assessed as induction of Ca2+ influx by scintillation counting
Agonist activity at human NK3R expressed in CHO cells assessed as induction of Ca2+ influx by scintillation counting
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[PMID: 25247671] |
| CHO | IC50 |
0.012 μM
Compound: [MePhe7]-NKB
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Displacement of [125I]His3, MePhe7 from human NK3R expressed in CHO cell membranes by scintillation counting
Displacement of [125I]His3, MePhe7 from human NK3R expressed in CHO cell membranes by scintillation counting
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[PMID: 25247671] |
| CHO | IC50 |
3 nM
Compound: 1a, [MePhe7]-NKB
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Displacement of ([125I]-His3, MePhe7)-NKB from NK3R (unknown origin) transfected in CHO cells by gamma counting analysis
Displacement of ([125I]-His3, MePhe7)-NKB from NK3R (unknown origin) transfected in CHO cells by gamma counting analysis
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[PMID: 23473945] |
| HEK293 | EC50 |
0.71 nM
Compound: [MePhe7]-NKB, [MePhe7]-Neurokinin B
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Agonist activity at wild type human NK3 receptor expressed in HEK293 cells assessed as [3H]IP accumulation after 45 mins
Agonist activity at wild type human NK3 receptor expressed in HEK293 cells assessed as [3H]IP accumulation after 45 mins
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[PMID: 22574973] |
| HEK293 | EC50 |
2.22 nM
Compound: [MePhe7]-NKB, [MePhe7]-Neurokinin B
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Agonist activity at human NK3 Y247F mutant expressed in HEK293 cells assessed as [3H]IP accumulation after 45 mins
Agonist activity at human NK3 Y247F mutant expressed in HEK293 cells assessed as [3H]IP accumulation after 45 mins
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[PMID: 22574973] |
| HEK293 | EC50 |
3.48 nM
Compound: [MePhe7]-NKB, [MePhe7]-Neurokinin B
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Agonist activity at human NK3 H316W mutant expressed in HEK293 cells assessed as [3H]IP accumulation after 45 mins
Agonist activity at human NK3 H316W mutant expressed in HEK293 cells assessed as [3H]IP accumulation after 45 mins
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[PMID: 22574973] |
Chemical Information
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CAS No. 110880-53-0
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Appearance Solid
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분자량 1272.49
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화학식 C60H81N13O14S2
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Color White to off-white
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Sequence
Asp-Met-His-Asp-Phe-Phe-{MePhe}-Gly-Leu-Met-NH2
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Sequence Shortening
DMHDFF-{MePhe}-GLM-NH2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
In Vitro:
DMSO : 20 mg/mL (15.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (0.98 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (0.98 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.7859 mL | 3.9293 mL | 7.8586 mL | 19.6465 mL |
| 5 mM | 0.1572 mL | 0.7859 mL | 1.5717 mL | 3.9293 mL | |
| 10 mM | 0.0786 mL | 0.3929 mL | 0.7859 mL | 1.9647 mL | |
| 15 mM | 0.0524 mL | 0.2620 mL | 0.5239 mL | 1.3098 mL |
[MePhe7]-Neurokinin B Related Classifications
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